1. Field of the Invention
The present invention relates to a novel organic substance included in the class comprising substituted or non-substituted isophthalic acid picolylamides, which is pharmacologically active and able to inhibit the blood platelet aggregation in vitro and in vivo and to control the thromboembolic disorders produced by a modified blood platelet reactivity.
The present invention also relates to a process for the synthesis of said substance.
The compound forming the object of the present invention is a 4-methoxy-isophthalic acid picolylamide whose chemical denomination is 3-carbamoyl(3'-picolyl)-4-methoxy-1-benzamide or, in an equivalent nomenclature, N-N'-(3'-picolyl)-4-methoxy-isophthalamide, the formula of which is C.sub.15 H.sub.15 N.sub.3 O.sub.3 corresponding to a mole weight of 285,3.
The conventional structural formula thereof can be represented as follows: ##STR2##
In the following description, the above defined compound will be briefly indicated as G 619.
2. Prior Art
It is well known, particularly from U.S. Pat. No. 3,973,026, Italian Pat. No. 1016005, U.S. Pat. No. 4,294,833 and German patent No. 3113150, that the organic compounds of the class comprising substituted or non-substituted isophthalic acid picolylamides show an anti-coagulant, fibrinolitic and blood platelet anti-aggregant activity. Among said compounds N-N'-bis-(3-picolyl)-4-methoxy-isophthalamide monohydrate under a crystal form has shown a particularly high activity (see German Pat. No. 3113150), which compound is briefly indicated with the denomination "picotamide monohydrate".
It has now been surprisingly found that the compound object of the present invention has a still higher and more rapid pharmacological activity of the same type, particularly as far as the inhibition of blood platelet aggregation is concerned. On the basis of the knowledge available at the state of the prior art for the compounds included in the above-mentioned class, and particularly for anhydrous picotamide and picotamide monohydrate, it was not to be expected as obvious that an elimination of the 3-picoline radical on the amide nitrogen atom in 1-position would produce a nett increase of the pharmacological activity and biodisposability, nor could it be expected that such activity increase would be free from negative side effects, as on the contrary it has resulted with the compound object of the present invention.